IP Library Patent Application 16877957
Patent Application
App. No. 16/877,957

DEPOT FORMULATIONS

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Patent No.
US None
App. No.
16/877,957
Abstract

Pharmaceutical compositions comprising an active pharmaceutical ingredient, a high viscosity liquid carrier material, a hydrophobic solvent, and a hydrophilic solvent are disclosed. Also disclosed are methods of manufacturing and using the compositions. The compositions are suitable for use, e.g., as depot formulations.

Claims (43)

1 . A composition comprising:

sirolimus present in an amount ranging from about 1 wt % to about 5 wt %, based on weight of the composition;

sucrose acetate isobutyrate (SAIB) present in an amount ranging from about 0.5 wt % to about 5 wt %, based on weight of the composition;

benzyl benzoate present in an amount ranging from about 35 wt % to about 50 wt %, based on weight of the composition;

ethanol present in an amount ranging from about 1 wt % to about 10 wt %, based on weight of the composition;

polyethylene glycol (PEG) present in an amount ranging from about 40 wt % to about 50 wt %, based on weight of the composition; and

vitamin E in an amount ranging from about 0.01 wt % to about 5 wt %.

2 .- 9 . (canceled)

10 . The composition of claim 1 , wherein the benzyl benzoate is present in an amount ranging from about 35 wt % to about 45 wt %, based on weight of the composition.

11 .- 15 . (canceled)

16 . The composition of claim 1 , wherein the ethanol is present in an amount ranging from about 1 wt % to about 7 wt %, based on weight of the composition.

17 .- 24 . (canceled)

25 . The composition of claim 1 , wherein the vitamin E is present in an amount ranging from about 0.1 wt % to about 5 wt %, based on weight of the composition.

26 . The composition of claim 1 , wherein the vitamin E is present in an amount ranging from about 0.5 wt % to about 2 wt %, based on weight of the composition.

27 . The composition of claim 1 , wherein the composition has a weight ratio of SAIB:vitamin E ranging from about 0.5 to about 10.

28 .- 29 . (canceled)

30 . The composition of claim 1 , the composition consisting essentially of:

sirolimus in an amount ranging from about 1 wt % to about 5 wt %, based on weight of the composition;

SAIB in an amount ranging from about 0.1 wt % to about 10 wt %, based on weight of the composition;

benzyl benzoate in an amount ranging from about 30 wt % to about 45 wt %, based on weight of the composition;

ethanol in an amount ranging from about 1 wt % to about 10 wt %, based on weight of the composition;

PEG400 in an amount ranging from about 40 wt % to about 50 wt %, based on weight of the composition; and

vitamin E in an amount ranging from about 0.5 wt % to about 2 wt %, based on weight of the composition.

31 .- 33 . (canceled)

34 . The composition of claim 1 , wherein the composition is pharmaceutically acceptable.

35 . A method of treating a subject afflicted with an eye condition, the method comprising:

administering a composition to an eye of a subject in need thereof, wherein the composition comprises an effective amount of an active pharmaceutical ingredient capable of treating the eye condition, the composition comprising:

an active pharmaceutical ingredient;

a high viscosity liquid carrier material (HVLCM);

a first hydrophobic solvent; and

a hydrophilic solvent.

36 . (canceled)

37 . The method of claim 35 , wherein the eye condition comprises uveitis, diabetic macular edema, or wet age-related macular degeneration.

38 . The method of claim 35 , wherein the administering comprises injecting.

39 . The composition of claim 1 , wherein the benzyl benzoate is present in an amount ranging from about 40 wt % to about 50 wt %, based on weight of the composition.

40 . The composition of claim 1 , wherein the ethanol is present in an amount ranging from about 3 wt % to about 10 wt %, based on weight of the composition.

41 . The composition of claim 1 , wherein a weight ratio of SAIB to vitamin E ranges from about 60:1 to about 1:2.

42 . The composition of claim 1 , wherein a weight ratio of SAIB to vitamin E ranges from about 10:1 to about 1:1.8.

43 . The composition of claim 1 , wherein a weight ratio of SAIB to vitamin E ranges from about 5:1 to about 1:1.5.

44 . The composition of claim 1 , wherein a weight ratio of SAIB to vitamin E ranges from about 2:1 to about 1:1.5.

45 . The composition of claim 1 , wherein the composition has a density at 25° C. and 1 atmosphere ranging from 1.02 g/mL to 1.15 g/mL.

46 . The composition of claim 1 , wherein the composition has a viscosity ranging from about 1 cP to about 150 cP at 25° C. and 1 atmosphere.

47 . The composition of claim 1 , wherein the vitamin E is present in an amount ranging from about 0.02 wt % to about 0.09 wt %, based on weight of the composition.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 19, 2020
From: TAMRAZ, WILMA; SU, HUEY-CHING; LIN, WEIQI; YAMADA, KAZUHITO; MATSUMOTO, NAOKI; MUDUMBA, SREENIVASU; OKABE, KOMEI
To: DURECT CORPORATION; SANTEN PHARMACEUTICAL CO., LTD.
Reel/Frame 052701/0652 →